Marimastat is a broad spectrum inhibitor of MMPs (IC50 values are 3, 5, 6, 9 and 13 nM for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 respectively). Inhibits peritoneal dissemination of human gastric cancer cells in vivo through inhibition of tumor angiogenesis.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Rasmussen and McCann (1997) Matrix metalloproteinase inhibition as a novel anticancer strategy: a review with special focus on batimastat and marimastat. Pharmacol.Ther. 75 69.
[2] Wada et al (2003) Reduced angiogenesis in peritoneal dissemination of gastric cancer through gelatinase inhibition. Clin.Exp.Metastasis 20 431.
[3] Chi-Li Chiu et. Al. Cell matrix remodeling ability shown by image spatial correlation. Journal of Biophysics, 2013, 532030 (2013).
分子式 C15H29N3O5 |
分子量 331.41 |
CAS号 154039-60-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO >20 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00002911 | Lung Cancer | Drug: marimastat | ILEX Oncology Services, Incorporated|National Cancer Institute (NCI) | Phase 3 | 1996-12-01 | 2013-12-17 |
NCT00003010 | Breast Cancer | Drug: marimastat | Eastern Cooperative Oncology Group|National Cancer Institute (NCI)|North Central Cancer Treatment Group | Phase 3 | 1997-09-01 | 2010-01-26 |
NCT00003011 | Lung Cancer | Drug: marimastat|Drug: Placebo | NCIC Clinical Trials Group|Canadian Cancer Trials Group | Phase 3 | 1997-03-01 | 2013-05-30 |
NCT00261391 | Vascular Anomalies | Drug: Marimastat | Boston Children Hospital | Phase 1 | 2000-10-01 | 2008-01-08 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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